牛血清白蛋白与十二烷基硫酸钠作用的机理

利用电动势法得到了牛血清白蛋白(BSA)与十二烷基硫酸钠(SDS)相互作用的结合等温线. 通过四阶导数紫外光谱法和荧光光谱法研究了相互作用过程中芳香族氨基酸残基微环境极性的变化. 通过研究发现, 随着SDS浓度的逐渐增大, SDS在BSA上的平均结合数(v)逐渐增大, 色氨酸(Trp)残基所处微环境的极性在减弱后保持基本不变, 酪氨酸残基所处微环境的极性在明显增强后稍有减弱, 苯丙氨酸残基所处微环境的极性略有增强. 结果表明, 当v由0增大到14时, SDS主要结合在BSA的Trp-213附近并逐渐形成聚集体, 从而诱导BSA由结构域ⅡA 开始逐渐展开. 此后, SDS呈正协同作用的特点与BSA 结合, v急剧增大. 当v约为302 时, SDS在BSA上的结合基本达到饱和, BSA的构象趋于稳定.     

胸腺素α1类似物的定点PEG修饰及其免疫活性评价

PEG修饰是改善蛋白质及肽类药物药代动力学特性的有效途径。然而与蛋白质相比,肽类化合物的分子较小,PEG的分子体积较大,其长链很可能会遮蔽肽的活性位点。因此,肽类化合物PEG修饰的位置和数量对于保持肽的生物活性至关重要。为阐明PEG修饰的位置与肽生物活性之间的关系,对肽类药物日达仙（胸腺素α1,Tα1）进行了定点修饰。Tα1具有α-螺旋、β-转角和无规卷曲的结构区域。分别在这些区域选择不同的位点进行PEG修饰。PEG的定点修饰是通过引入Cys,利用其-SH与mPEG-MAL的特异性反应而实现的。Con A刺激下的脾细胞产生IFN-γ试验的初步结果表明,PEG修饰对活性的影响与修饰的位置有一定的关系,大多数情况下,PEG修饰能保持Tα1的免疫活性。PEG修饰的位点对于保持肽的生物活性是很重要的。     

环境卫星HJ1A超光谱成像仪在轨辐射定标及光谱响应函数敏感性分析

环境卫星HJ1A搭载的超光谱成像仪HSI是我国第一个对地观测的星载高光谱传感器,针对超光谱成像仪缺乏各通道光谱响应函数这一问题,对传统的反射率基法予以改进,提出一种不使用光谱响应函数的场地定标方法。利用敦煌场地2009年8月定标实验数据,实现超光谱成像仪在轨辐射定标。通过构建不同形状的光谱响应函数,分析光谱响应函数形状对最终辐射定标结果产生的误差。结果表明,利用新提出的场地定标方法可以实现超光谱成像仪绝对辐射定标,除水汽和氧气吸收通道外,光谱响应函数对定标结果的影响小于3％,采用新定标方法得到的定标系数可以满足应用的需求。     

兴国红鲤成熟卵子精孔器及精子进入区的扫描电镜研究

用扫描电镜详细观察了兴国红鲤成熟卵子动物极方向卵膜上的精孔器(Micropylar Apparatus)及其正下方位于卵子质膜表面的精子进入区(Sperm Entry Site)的微细结构。精孔器为漏斗型结构;精子进入区由卵子质膜表面特化而成,可区分为精子依附位点和精子入卵位点。研究表明,精孔器的     

Interactions of Human Serum Albumin with Phenothiazine Drugs: Insights from Fluorescence Spectroscopic Studies

This study was based on the use of fluorescence quenching and differentiation between static and dynamic quenching, as well as energy transfer for distance measurements. The interactions of human serum albumin with phenothiazine drugs, i.e. phenothiazine, chlorpromazine, perphenazine and promethazine, were studied and extrapolated important information on quenching mechanism, types of interaction force, binding‐site number and distance between Trp214 in HSA and the bound drugs. This study has great significance in methodology and understanding the protein‐drug interaction mechanism.     

Statistical theory of multiple-site linear wall-adsorption capillary Chromatography

Based on the mass-balance principle, a particular diffusion equation to describe the movement of solute molecules in the stagnant layer of multiple-site solid surfaces is constructed. From the equation, the moments of residence time in a step on multiple-site surfaces are derived. Similarly, the moments in a step in the mobile phase are also derived from a diffusion-drift equation. According to the probability theory, there exists a general relationship between the moments of an elution curve and the moments in a step. Through this relationship, the expressions of the elution-curve moments are derived from the step moments. In this paper, the details related to multiple-site linear wall-adsorption capillary chromatography are described and added in the equations to determine the step moments. The resultant expressions of the elution-curve moments involve various factors, such as adsorption–desorption rate constants, equilibrium constants, axial and radial dispersions in the mobile phase. Afterwards, the moment expressions are used to analyze the peak tailing. The results show that a small quantity of sites with a slow desorption rate will lead to a large peak asymmetry.     

A concise and efficient synthesis of flumazenil and its precursor for radiolabeling with fluorine-18

Presently there is a strong interest in developing radioligands for in vivo imaging the GABA_A-Bz site with positron emission tomography (PET). Flumazenil (1), a high-affinity GABA_A-Bz site inverse agonist, is amenable for ¹¹C and ¹⁸F-labeling. The current methods for synthesis of 1 and its precursor for ¹⁸F-labeling are not ideal and restrict structure-activity relationship (SAR) development. Herein we present a novel and less troublesome synthesis of 1 and its cognates to aid in the development of improved radioligands for PET imaging of GABA_A-Bz site.     

Characteristics of photoluminescence, thermoluminescence and thermal degradation in Eu-doped BaMgAl10O17 and SrMgAl10O17

The relation between photoluminescence and thermoluminescence from Eu-doped BAM (BaMgAl₁₀O₁₇) and SAM (SrMgAl₁₀O₁₇) are investigated. The emission peak of SAM:Eu shifts from 463 to 489 nm whereas that of BAM:Eu only shifts 3 nm at 450 nm as temperature decreased from 300 to 50 K under 146 nm excitation. This can be explained by the fact that there are Beevers–Ross (BR) and mid-oxygen (mO) sites for Eu ions in SAM. The emission peak around 463 nm from SAM:Eu is ascribed to Eu ions in the mO site, while the peak around 489 nm is ascribed to ones in the BR site in SAM host. From the result of thermal degradation of SAM:Eu, it is confirmed that the Eu ions located at mO site are easy to degrade compared with those located at BR site. The thermal degradation of BAM:Eu phosphor becomes large with the increase in Eu concentration. We suggest that the thermal degradation of BAM:Eu phosphor is due to the tendency of Eu ions to occupy the mO site.